dhodhin3

DHODH-IN-3 is an effective inhibitor of human dihydroorotate dehydrogenase (HsDHODH) with IC50 value of 261 nM. DHODH-IN-3 binds to the ubiquinone binding cavity in DHODH with a Kiapp of 32 nM. DHODH-IN-3 has the potential to treat malaria.

hDHODH-IN-3 is an inhibitor of human dihydroorotate dehydrogenase with a pMIC50 value of 8.6. hDHODH-IN-3 can inhibit measles virus replication.

DHODH-IN-31 is a human dihydroorotate dehydrogenase (DHODH) inhibitor with an IC50 of 0.59 μM. DHODH-IN-31 exhibits antiviral activity, enabling research into infectious diseases such as SARS-CoV-2 and facilitating the development of antiviral therapeutics and mechanistic studies of nucleotide biosynthesis pathways in human cells.

DHODH-IN-30 (compound 4g) is a potent inhibitor of human dihydroorotate dehydrogenase (hDHODH), with an IC50 of 32 nM. Additionally, DHODH-IN-30 offers protective effects against oxidative stress.

DHODH-IN-32 (Compound A1) is a DHODH inhibitor demonstrating significant cytotoxicity against the NCI-60 cell lines, with particular sensitivity observed in breast cancer, prostate cancer, and leukemia cell lines. It induces apoptosis by activating the Caspase pathway and causes cell cycle arrest at the G0/G1 phase while generating ROS to inhibit cellular metabolism. In a mouse breast cancer model, DHODH-IN-32 exhibits notable antitumor properties and may be utilized for breast cancer research.

DHODH-IN-33 is a selective DHODH inhibitor that exhibits potent activity against A549 cells (IC50 = 5.22 μM) and 5637 cells (IC50 = 3.03 μM). It induces autophagy-dependent ferroptosis, characterized by mitochondrial dysfunction, lipid peroxidation, and accumulation of ROS, without significant toxicity in vivo. The anticancer effect of DHODH-IN-33 is achieved through promoting autophagy-dependent degradation of dihydroorotate dehydrogenase. This compound can be used in studies related to non-small cell lung cancer and bladder cancer.

RORγt/DHODH-IN-3 (compound (S)-14d) is a potent, orally active dual inhibitor of RORγt (IC50: 0.098 μM) and DHODH (IC50: 0.432 μM) with significant in vivo anti-inflammatory effects.